文献类型：期刊文献

英文题名：Quaternized Polysaccharide-Based Cationic Micelles as a Macromolecular Approach to Eradicate Multidrug-Resistant Bacterial Infections while Mitigating Antimicrobial Resistance

作者：Xie, Fang[1];Jiang, Lai[2];Xiao, Ximian[3];Lu, Yiwen[1];Liu, Runhui[3];Jiang, Wei[2];Cai, Jie[1,4]

机构：[1]Wuhan Univ, Coll Chem & Mol Sci, Hubei Engn Ctr Nat Polymers Based Med Mat, Wuhan 430072, Peoples R China;[2]Wuhan Univ, Zhongnan Hosp, Med Res Inst, Dept Biol Repositories,Frontier Sci Ctr Immunol &, Wuhan 430071, Peoples R China;[3]East China Univ Sci & Technol, Sch Mat Sci & Engn, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[4]Wuhan Univ, Res Inst Shenzhen, Shenzhen 518057, Peoples R China

年份：2022

卷号：18

期号：12

外文期刊名：SMALL

收录：;EI(收录号：20220711636518);WOS:【SCI-EXPANDED(收录号:WOS:000751841500001)】；

基金：F. X., L. J., and X. X. contributed equally to this work. F.X. and X.X. performed antibacterial experiments. F.X. and L.J. performed in vivo experiments. F.X., L.J. and W.J. interpreted in vivo results. F.X. and Y.L. performed the preparation and characterization of the samples. R.L. advised on antibacterial tests, discussed the antibacterial results. F.X., L.J. and J.C. wrote the paper. J.C. directed the overall project. All authors discussed the results. This research was funded by the National Natural Science Foundation of China (52173105, 21875170). The authors thank to the facility support of the Basic Research Program of Central Government Funds for Shenzhen Science and Technology Development (JCYJ20180507184711069,JCYJ20170818112409808), Shenzhen Fundamental Research Program (2021Szvup099), and the Key Research and Development Program of Hubei Province (2020BCA079, 2018ACA159). All experimental protocols on animals were approved and pe rformed in accordance with the guidelines of the Animal Ethics Committee of Wuhan University.

语种：英文

外文关键词：multidrug-resistant infection; polysaccharides; quaternization; wound healing

摘要：Microbial infections and microbial resistance lead to a high demand for new antimicrobial agents. Quaternized polysaccharides are cationic antimicrobial candidates; however, the limitation of homogeneous synthesis solvents that affect the molecular structure and biological activities, as well as their drug resistance remains unclear. Therefore, the authors homogeneously synthesize a series of quaternized chitin (QC) and quaternized chitosan (QCS) derivatives via a green and effective KOH/urea system and investigate their structure-activity relationship and biological activity in vivo and in vitro. Their study reveals that a proper match of degree of quaternization (DQ) and degree of deacetylation (DD ') of QC or QCS is key to balance antimicrobial property and cytotoxicity. They identify QCS-2 as the optimized antimicrobial agent with a DQ of 0.46 and DD ' of 82%, which exhibits effective broad-spectrum antimicrobial properties, good hemocompatibility, excellent cytocompatibility, and effective inhibition of bacterial biofilm formation and eradication of mature bacterial biofilms. Moreover, QCS-2 exhibits a low propensity for development of drug resistance and significant anti-infective effects on MRSA in vivo comparable to that of vancomycin, avoiding excessive inflammation and promoting the formation of new blood vessels, hair follicles, and collagen deposition to thus expedite wound healing.